Assay Detail
Binding
CHEMBL3820514
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human N-terminal GST-tagged TTK using biotinylated PWDPDDADITEILG as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by TR-FRET assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.78 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422104 | — | — | 1 | 9.00 |
| CHEMBL3819182 | — | — | 1 | 8.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422104 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3819182 | — | IC50 | = | 2.8 | nM | 8.55 |